Epigenetic Reader Domain Inhibitor

KG-501 (Standard) is the analytical standard of KG-501 (HY-103299). This product is intended for research and analytical applications. KG-501 is a CREB inhibitor, with an IC₅₀ of 6.89 μM.

NVS-CECR2-1 (Standard) is the analytical standard of NVS-CECR2-1 (HY-110374). This product is intended for research and analytical applications. NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC₅₀=47 nM; K_d=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism. NVS-CECR2-1 is a chemical probe.

GNE-272 (Standard) is the analytical standard of GNE-272 (HY-100726). This product is intended for research and analytical applications. GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300.

Hexamethylene bisacetamide (Standard) is the analytical standard of Hexamethylene bisacetamide. This product is intended for research and analytical applications. Hexamethylene bisacetamide (HMBA) is a differentiation inducer and selective bromine domain inhibitor that can differentiate across the blood-brain barrier. Hexamethylene bisacetamide can induce tumor cell differentiation and inhibit cell proliferation, showing antitumor activity. Hexamethylene bisacetamide induces apoptosis by Notch1, Bcl-2 and p53 signaling pathways. In addition, Hexamethylene bisacetamide improves the obesity phenotype of mice.

RMM23 is an inhibitor targeting PfBDP1 with a K_d value of 1.24 μM. RMM23 against the wild-type strains 3D7 and NF54, and the multidrug-resistant K1 strain in vitro blood stage, with EC₅₀ values of 18 μM, 14 μM, 20 μM, respectively .

(+)-JQ-1 (Standard) is the analytical standard of (+)-JQ-1 (HY-13030). This product is intended for research and analytical applications. (+)-JQ-1 (JQ1), a chemical probe, is a potent, specific, CNS-penetrant and reversible BET bromodomain inhibitor, with IC₅₀s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.

Alobresib (Standard) is the analytical standard of Alobresib (HY-109050). This product is intended for research and analytical applications. Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research.

Inobrodib (Standard) is the analytical standard of Inobrodib (HY-111784). This product is intended for research and analytical applications. Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the p300/CBP bromodomain. Inobrodib binds to p300 and CBP with K_d values of 1.3 and 1.7 nM, respectively, and with 170/130-fold selectivity compared with BRD4 with a K_d of 222 nM. CCS1477 inhibits cell proliferation in prostate cancer cell lines and decreases androgen receptor (AR)- and C-MYC-regulated gene expression.

AZD5153 (6-Hydroxy-2-naphthoic acid) (Standard) is the analytical standard of AZD5153 (6-Hydroxy-2-naphthoic acid) (HY-100653A). This product is intended for research and analytical applications. AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM.

MI-2-2 (Standard) is the analytical standard of MI-2-2 (HY-108350). This product is intended for research and analytical applications. MI-2-2 is a potent menin-MLL inhibitor. MI-2-2 binds to menin with low nanomolar affinity (K_d=22nM) and very effectively disrupts the bivalent protein-protein interaction between menin and MLL. MI-2-2 has specific and very pronounced activity in MLL leukemia cells, including inhibition of cell proliferation, down-regulation of Hoxa9 expression, and differentiation.

CBP/p300-IN-1 (Standard) is the analytical standard of CBP/p300-IN-1 (HY-111420). This product is intended for research and analytical applications. CBP/p300-IN-1 is a CBP/EP300 bromodomain inhibitor.

EP300/CBP-IN-1 (compound 172) is a potent EP300/CBP inhibitor with IC₅₀s of 2.3 nM and 2.1 nM for CBP BRD and EP300 BRD, respectively. EP300/CBP-IN-1 has the inhibitory effect on the proliferation of prostate cancer CWR22RV1 cells.

SNIPER(BRD)-1 (Standard) is the analytical standard of SNIPER(BRD)-1 (HY-111875). This product is intended for research and analytical applications. SNIPER(BRD)-1 is a SNIPER degrader of BRD4, cIAP1 and XIAP. SNIPER(BRD)-1 has IC₅₀ values of 6.8 nM, 17 nM and 49 nM for cIAP1, cIAP2 and XIAP, respectively. SNIPER(BRD)-1 can be used for cancer research. (Blue: LCL161 (HY-15518); Black: linker (HY-W008005); Pink: (+)-JQ-1 (HY-13030))

GSK6853 (Standard) is the analytical standard of GSK6853 (HY-100220). This product is intended for research and analytical applications. GSK6853, a chemical probe, is a potent and selective inhibitor of the BRPF1 bromodomain. GSK6853 shows excellent BRPF1 potency (pKd = 9.5) and greater than 1600-fold selectivity over all other bromodomains.

C646 (Standard) is the analytical standard of C646 (HY-13823). This product is intended for research and analytical applications. C646 is a selective and competitive histone acetyltransferase p300 inhibitor with K_i of 400 nM, and is less potent for other acetyltransferases.

TPOP146 (Standard) is the analytical standard of TPOP146 (HY-100697). This product is intended for research and analytical applications. TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.

5-Ph-IAA (Standard) is the analytical standard of 5-Ph-IAA (HY-134653). This product is intended for research and analytical applications. 5-Ph-IAA is a derivative of IAA. 5-Ph-IAA, a ligand, establishes the auxin-inducible degron 2 (AID2) system together with an OsTIR1 (F74G) mutant. AID2 induces rapid and efficient depletion of mAID-fused proteins to study protein function in living cells, causing tumor suppression.

TP-472 (Standard) is the analytical standard of TP-472 (HY-100517). This product is intended for research and analytical applications. TP-472, a chemical probe, is a selective BRD9/7 inhibitor, with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7. TP-472 induces apoptosis of melanoma cells.

BAY-299 (Standard) is the analytical standard of BAY-299 (HY-107424). This product is intended for research and analytical applications. BAY-299, a chemical probe, is a very potent, dual inhibitor with IC₅₀s of 67 nM for BRPF2 bromodomains (BD), 8 nM for TAF1 BD2, and 106 nM for TAF1L BD2.

Y06137 (Standard) is the analytical standard of Y06137 (HY-111503). This product is intended for research and analytical applications. Y06137 is a potent and selective BET inhibitor for treatment of castration-resistant prostate cancer (CRPC). Y06137 binds to the BRD4(1) bromodomain with a K_d of 81 nM.